Thiazolidone derivatives as inhibitors of chikungunya virus

Surender Singh Jadav, Barij Nayan Sinha, Rolf Hilgenfeld, Boris Pastorino, Xavier De Lamballerie*, Venkatesan Jayaprakash

*Corresponding author for this work
18 Citations (Scopus)

Abstract

A series of arylalkylidene derivatives of 1,3-thiazolidin-4-one (1-20) were synthesized and tested for their antiviral activity against chikungunya virus (LR2006-OPY1) in Vero cell culture by CPE reduction assay. Five compounds (7-9, 16 and 19) were identified to have anti-ChikV activity at lower micro molar concentration. The compounds 7, 8, 9, 16 and 19 inhibited the virus at 0.42, 4.2, 3.6, 40.1 and 6.8 μM concentrations respectively. Molecular docking simulation has been carried out using the available X-ray crystal structure of the ChikV nsp2 protease, in order to elucidate the possible mechanism of action. Interaction of ligands with ChikV nsp2 protease (PDB Code: 3TRK) suggested the possible mechanism of protease inhibition to act as potent anti-ChikV agents.

Original languageEnglish
JournalEuropean Journal of Medicinal Chemistry
Volume89
Pages (from-to)172-178
Number of pages7
ISSN0223-5234
DOIs
Publication statusPublished - 01.01.2014

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